Table 3.
Permeability results (Pe, 10−6 cm/s) from the PAMPA–BBB assay for compounds 12, 20–24, 30–38, and 52 and their prediction of BBB penetration.
Compd. | Pe (10−6 cm/s)a | Predictionb |
---|---|---|
NTZ | 1.26±0.21 | CNS+/− |
12 | 5.76±0.57 | CNS+ |
20 | 0.45±0.03 | CNS− |
21 | 0.09±0.01 | CNS− |
22 | 6.02±0.27 | CNS+ |
23 | 4.92±0.31 | CNS+ |
24 | 12.62±1.22 | CNS+ |
30 | 5.76±0.55 | CNS+ |
31 | 3.42±0.07 | CNS+ |
32 | 6.16±0.50 | CNS+ |
33 | 10.41±1.25 | CNS+ |
34 | 6.82±0.50 | CNS+ |
35 | 9.24±0.47 | CNS+ |
36 | 10.62±0.10 | CNS+ |
37 | 9.89±0.37 | CNS+ |
38 | 9.88±0.75 | CNS+ |
52 | 10.50±1.13 | CNS+ |
Values are expressed as the mean ± SD (n ≥ 3).
Compounds with permeabilities Pe > 3.08 × 10−6 cm/s could cross the BBB by passive diffusion (CNS+). Compounds with Pe < 1.13 × 10−6 cm/s show low BBB permeation (CNS−), and compounds with 1.13 × 10−6 cm/s < Pe < 3.08 × 10−6 cm/s show uncertain BBB permeation (CNS+/−).